JZL 184|1101854-58-3|-陌孚医药/Medlife

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JZL 184

目录号: PL06913 纯度: ≥98%

CAS No. :1101854-58-3

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中文名称	JZL 184
中文别名	JZL184 抑制剂;JZL 184
英文名称	JZL 184
英文别名	(4-nitrophenyl) 4-[bis(1,3-benzodioxol-5-yl)-hydroxymethyl]piperidine-1-carboxylate;4-nitrophenyl-4-[bis(1,3-benzodioxol-5-yl)(hydroxy)methyl]piperidine-1-carboxylate;KB-78010;CTK8E9996;CHEBI:674401;4-nitrophenyl 4-(di(benzo[d][1,3]dioxol-5-yl)(hydroxy)methyl)piperidine-1-carboxylate;UNII-7MZ1I2J68A;JZL184;4-nitrophenyl 4-(dibenzo[d][1,3]dioxol-5-yl(hydroxy)methyl)piperidine-1-carboxylate;4-nitrophenyl 4-(dibenzo[d][1,3]dioxol-5-ylhydroxymethyl)piperidine-1-carboxylate;JZL-184;CHEMBL576786;JZL 184 JZL184 JZL-184;4-[Bis(1,3-benzodioxol-5-yl)hydroxymethyl]-1-piperidinecarboxylic acid 4-nitrophenyl ester;JZL 184;7MZ1I2J68A;4-nitrophenyl 4-[bis(2H-1,3-benzodioxol-5-yl)(hydroxy)methyl]piperidine-1-carboxylate;BDBM50300355;1-Piperidinecarboxylic acid, 4-(bis(1,3-benzodioxol-5-yl)hydroxymethyl)-, 4-nitrophenyl ester;1-Piperidinecarboxylic acid, 4-[bis(1,3-benzodioxol-5-yl)hydroxymethyl]-, 4-nitrophenyl ester;GTPL5207;BDBM60622
Cas No.	1101854-58-3
分子式	C₂₇H₂₄N₂O₉
分子量	520.49
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	JZL 184 是一种有效的，选择性的且不可逆的 MAGL 抑制剂，可阻断脑膜中的 2-花生四烯酸甘油酯 (2-AG) 的水解 (IC₅₀ 为 8 nM)。JZL 184 对 MAGL 的选择性比 FAAH 高 300 倍以上。
生物活性	JZL 184 is a potent, selective and irreversible MAGL inhibitor that blocks 2-Arachidonoylglycerol (2-AG) hydrolysis in brain membranes (IC 50 of 8 nM). JZL 184 displays >300-fold selectivity for MAGL over FAAH.
性状	Solid
IC50 & Target[1][2]	IC50: 8 nM (2-Arachidonoylglycerol (2-AG) hydrolysis)
体外研究(In Vitro)	JZL 184 displays IC50 values of 8 nM and 4 μM for blockade of 2-AG and oleamide (FAAH substrate) hydrolysis in brain membranes, respectively. Comparable inhibitory effects are observed with recombinant MAGL and FAAH when expressed in COS7 cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	JZL 184 (4-40 mg/kg; intraperitoneal injection; once; C57Bl/6 mice) treatment produces a rapid and sustained blockade of brain 2-AG hydrolase activity in mice, resulting in 8-fold elevations in endogenous 2-AG levels that are maintained for at least 8 h. JZL 184-treated mice shows a remarkable array of CB1-dependent behavioral effects, including analgesia, hypomotility, and hypothermia. JZL 184 prolongs depolarization-induced suppression of excitation (DSE) in Purkinje neurons in cerebellar slices and DSE inhibition (DSI) in CA1 pyramidal neurons in hippocampal slices. JZL 184 produces greater enhancement of DSE/DSI in mouse neurons than that in rat neurons. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Long JZ, et al. Selective blockade of 2-arachidonoylglycerol hydrolysis produces cannabinoid behavioral effects. Nat Chem Biol. 2009 Jan;5(1):37-44. [2]. Pan B, et al. Blockade of 2-arachidonoylglycerol hydrolysis by selective monoacylglycerol lipase inhibitor 4-nitrophenyl 4-(dibenzo[d][1,3]dioxol-5-yl(hydroxy)methyl)piperidine-1-carboxylate (JZL184) Enhances retrograde endocannabinoid signaling. J Pharma

溶解度数据	In Vitro: DMSO : ≥ 35 mg/mL (67.24 mM)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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